SG2014012108A - 2 -amino-4 -(pyridin-2-yl)-5, 6-dihydro-4h-1, 3-oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors - Google Patents

2 -amino-4 -(pyridin-2-yl)-5, 6-dihydro-4h-1, 3-oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors

Info

Publication number
SG2014012108A
SG2014012108A SG2014012108A SG2014012108A SG2014012108A SG 2014012108 A SG2014012108 A SG 2014012108A SG 2014012108 A SG2014012108 A SG 2014012108A SG 2014012108 A SG2014012108 A SG 2014012108A SG 2014012108 A SG2014012108 A SG 2014012108A
Authority
SG
Singapore
Prior art keywords
bace
pyridin
dihydro
inhibitors
amino
Prior art date
Application number
SG2014012108A
Inventor
Rainer Martin Lueoend
Rainer Machauer
Heinrich Rueeger
Siem Jacob Veenstra
Original Assignee
Novartis Ag
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47018309&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=SG2014012108(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of SG2014012108A publication Critical patent/SG2014012108A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5355Non-condensed oxazines and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/48Drugs for disorders of the endocrine system of the pancreatic hormones
    • A61P5/50Drugs for disorders of the endocrine system of the pancreatic hormones for increasing or potentiating the activity of insulin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
SG2014012108A 2011-08-25 2012-08-23 2 -amino-4 -(pyridin-2-yl)-5, 6-dihydro-4h-1, 3-oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors SG2014012108A (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161527172P 2011-08-25 2011-08-25
US201261665395P 2012-06-28 2012-06-28
PCT/IB2012/054269 WO2013027188A1 (en) 2011-08-25 2012-08-23 2 -amino-4 - (pyridin- 2 -yl) - 5, 6 -dihydro-4h- 1, 3 -oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors

Publications (1)

Publication Number Publication Date
SG2014012108A true SG2014012108A (en) 2014-05-29

Family

ID=47018309

Family Applications (1)

Application Number Title Priority Date Filing Date
SG2014012108A SG2014012108A (en) 2011-08-25 2012-08-23 2 -amino-4 -(pyridin-2-yl)-5, 6-dihydro-4h-1, 3-oxazine derivatives and their use as bace-1 and/or bace - 2 inhibitors

Country Status (28)

Country Link
US (2) US9163011B2 (en)
EP (2) EP2748162B1 (en)
JP (1) JP5816369B2 (en)
KR (1) KR101601571B1 (en)
CN (1) CN103906748B (en)
AP (1) AP2014007507A0 (en)
AR (1) AR087668A1 (en)
AU (1) AU2012298177B2 (en)
BR (1) BR112014004131A2 (en)
CA (1) CA2845093A1 (en)
CL (1) CL2014000458A1 (en)
CO (1) CO6890097A2 (en)
CR (1) CR20140084A (en)
EA (1) EA024580B1 (en)
ES (2) ES2565229T3 (en)
GT (1) GT201400031A (en)
HK (1) HK1195903A1 (en)
IL (1) IL230975A0 (en)
MA (1) MA35356B1 (en)
MX (1) MX339303B (en)
PE (1) PE20141540A1 (en)
PL (1) PL2748162T3 (en)
SG (1) SG2014012108A (en)
TN (1) TN2014000062A1 (en)
TW (1) TW201313706A (en)
UY (1) UY34278A (en)
WO (1) WO2013027188A1 (en)
ZA (1) ZA201401139B (en)

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EP2663561B1 (en) 2011-01-13 2016-03-16 Novartis AG Novel heterocyclic derivatives and their use in the treatment of neurological disorders
WO2014065434A1 (en) * 2012-10-24 2014-05-01 Shionogi & Co., Ltd. Dihydrooxazine or oxazepine derivatives having bace1 inhibitory activity
EP2961749B1 (en) * 2013-03-01 2019-10-09 Amgen Inc. Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
CA2903215C (en) 2013-03-08 2021-07-20 Amgen Inc. Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
MA38556A1 (en) * 2013-04-11 2017-09-29 Hoffmann La Roche Inhibitors of bace1
JO3318B1 (en) 2013-06-18 2019-03-13 Lilly Co Eli Bace inhibitors
US20170066741A1 (en) 2014-02-19 2017-03-09 H. Lundbeck A/S 2-Amino-3,5,5-Trifluoro-3,4,5,6-Tetrahydropyridines as BACE1 Inhibitors for Treatment of Alzheimer's Disease
TW201623295A (en) 2014-04-11 2016-07-01 塩野義製藥股份有限公司 Dihydrothiazine and dihydrooxazine derivatives having BACE1 inhibitory activity
US9550762B2 (en) 2014-08-08 2017-01-24 Amgen, Inc. Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
JO3458B1 (en) 2014-11-10 2020-07-05 H Lundbeck As 2-Amino-6-(difluoromethyl)- 5,5-difluoro-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors
MA40941A (en) 2014-11-10 2017-09-19 H Lundbeck As 2-AMINO-5,5-DIFLUORO-6- (FLUOROMETHYL) -6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINES AS BACE1 INHIBITORS
CR20170187A (en) 2014-11-10 2018-02-01 H Lundbeck As 2-Amino-3,5-difluoro-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors for the treatment of Alzheimer's disease
CA2977264C (en) * 2015-02-25 2021-12-07 Teva Pharmaceuticals International Gmbh Use of pridopidine to improve cognitive function and for treating alzheimer's disease
US11471449B2 (en) 2015-02-25 2022-10-18 Prilenia Neurotherapeutics Ltd. Use of pridopidine to improve cognitive function and for treating Alzheimer's disease
TW201717948A (en) 2015-08-10 2017-06-01 H 朗德貝克公司 Combination treatment comprising administration of 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahydropyridines
PE20181015A1 (en) 2015-08-12 2018-06-26 H Lundbeck As 2-AMINO-3-FLUORO-3- (FLUOROMETHYL) -6-METI-6-PHENYL-3,4,5,6-TETRAHYDROPYRIDINES AS BACE1 INHIBITORS
JP6616525B2 (en) * 2016-03-01 2019-12-04 エフ.ホフマン−ラ ロシュ アーゲー BACE1 inhibitor
WO2018112081A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Oxazine derivatives as beta-secretase inhibitors and methods of use
EP3555106B1 (en) 2016-12-15 2022-03-09 Amgen Inc. Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use
EP3555085B1 (en) 2016-12-15 2020-12-02 Amgen Inc. Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use
CA3047288A1 (en) 2016-12-15 2018-06-21 Amgen Inc. Thiazine derivatives as beta-secretase inhibitors and methods of use
US11021493B2 (en) 2016-12-15 2021-06-01 Amgen Inc. 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use
AU2019258575A1 (en) 2018-04-27 2020-10-29 Shionogi & Co., Ltd. Tetrahydropyranooxazine derivatives having selective BACE1 inhibitory activity
CN109725092A (en) * 2019-03-19 2019-05-07 北京和合医学诊断技术股份有限公司 Detect the liquid phase chromatography analytical method of Ziprasidone content in blood
CN113173852B (en) * 2021-04-26 2022-07-12 深圳市华先医药科技有限公司 Preparation method of difluoro malonate type compound

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Also Published As

Publication number Publication date
EP3023423B1 (en) 2017-05-31
TN2014000062A1 (en) 2015-07-01
JP2014524463A (en) 2014-09-22
KR101601571B1 (en) 2016-03-08
MX339303B (en) 2016-05-19
EA024580B1 (en) 2016-09-30
IL230975A0 (en) 2014-03-31
MX2014002230A (en) 2014-04-25
GT201400031A (en) 2015-02-19
US20150150877A1 (en) 2015-06-04
AU2012298177B2 (en) 2015-10-29
KR20140054313A (en) 2014-05-08
CR20140084A (en) 2014-05-02
US20130172331A1 (en) 2013-07-04
ES2638832T3 (en) 2017-10-24
AR087668A1 (en) 2014-04-09
UY34278A (en) 2013-04-05
US9163011B2 (en) 2015-10-20
JP5816369B2 (en) 2015-11-18
CA2845093A1 (en) 2013-02-28
CO6890097A2 (en) 2014-03-10
CN103906748B (en) 2017-06-16
PE20141540A1 (en) 2014-10-31
WO2013027188A1 (en) 2013-02-28
EA201490491A1 (en) 2014-06-30
PL2748162T3 (en) 2016-06-30
ZA201401139B (en) 2014-12-23
NZ621093A (en) 2015-05-29
BR112014004131A2 (en) 2017-06-13
ES2565229T3 (en) 2016-04-01
EP2748162A1 (en) 2014-07-02
EP2748162B1 (en) 2015-12-16
TW201313706A (en) 2013-04-01
CN103906748A (en) 2014-07-02
EP3023423A1 (en) 2016-05-25
AP2014007507A0 (en) 2014-03-31
AU2012298177A1 (en) 2014-03-06
MA35356B1 (en) 2014-08-01
CL2014000458A1 (en) 2014-09-05
HK1195903A1 (en) 2014-11-28

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